| Literature DB >> 20833039 |
Chih-Hung Chen1, On Lee, Chung-Niang Yao, Meng-Yun Chuang, Yow-Lone Chang, May-Hua Chang, Yen-Fang Wen, Wan-Hsu Yang, Ching-Huai Ko, Nien-Tzu Chou, Mai-Wei Lin, Chin-Pen Lai, Chung-Yuan Sun, Ling-mei Wang, Yen-Chun Chen, Tzong-Hsiung Hseu, Chia-Ni Chang, Hui-Chun Hsu, Hui-Chi Lin, Yu-Li Chang, Ying-Chu Shih, Shuen-Hsiang Chou, Yi-Ling Hsu, Hsiang-Wen Tseng, Chih-Peng Liu, Chia-Mu Tu, Tsan-Lin Hu, Yuan-Jang Tsai, Ting-Shou Chen, Chih-Lung Lin, Shu-Jiau Chiou, Chung-Cheng Liu, Chrong-Shiong Hwang.
Abstract
A series of azulene-based derivatives were synthesized as potent inhibitors for receptor tyrosine kinases such as FMS-like tyrosine kinase 3 (FLT-3). Systematic side chain modification of prototype 1a was carried out through SAR studies. Analogue 22 was identified from this series and found to be one of the most potent FLT-3 inhibitors, with good pharmaceutical properties, superior efficacy, and tolerability in a tumor xenograft model.Entities:
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Year: 2010 PMID： 20833039 DOI： 10.1016/j.bmcl.2010.08.025
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823